BAZ1A-IN-1 是BAZ1A(含溴结构域蛋白)抑制剂(Kd:0.52 μM)。它对低表达BAZ1A的癌细胞表现出弱活性或无活性,但对高表达BAZ1A的癌细胞系显示出良好的抗生存作用。
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描述
BAZ1A-IN-1 is a potent BAZ1A inhibitor with the KD value of 0.52 μM for the BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-survival activity against cancer cell lines with high BAZ1A expression, but weak or no activity against cancer cells with low BAZ1A expression.
体外活性
Administration of BAZ1A-IN-1 (0.015-100?μM; 96 hours) exhibits good anti-viability activity against all the four cancer cell lines that have a high expression level of BAZ1A, with IC50 values of 5.08 μM, 4.29 μM, 10.65 μM, and 7.70 μM for THP-1, ZR-75-30, BT474, and H1975 cells, respectively[1].
Cas No.
941521-45-5
分子式
C32H24N8O6S2
分子量
680.71
储存和溶解度
DMSO:80 mg/mL (235.05 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years